The chemistry of quinolones has been reviewed by D. Bouzard in "Recent Advances in the Chemistry of Quinolones" in Recent Progress in the Chemical Synthesis of Antibiotics by Federico Arcamone, Springer-Verlag, 1990, p. 249-283. Articles by Peterson L. P., Quinolone Resistance in Clinical Practice: Occurrence and Importance, In Quinolone Antimicrobial Agents, 2nd edition; and by Moellering, R. C., Jr. Quinolones Antimicrobial Agents: Overview and Conclusion. American Society for Microbiology: Washington, D.C., 1993 pp 527-535 have been published emphasising the antibacterial and pharmacological properties of quinolones.
Norfloxacin, 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3 quinolinecarboxylic acid, is a fluorinated quinolone antibacterial agent and it's pharmacokinetics and antibacterial properties have been reported by B. Holmes et. al., Drugs, 30, 482-513 (1985); R. C. Rowen et. al., Pharmacotherapy 7, 92-110 (1987). ##STR6##
Ciprofloxacin, 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarb oxylic acid, is an analogue of norfloxacin. The antibacterial activity, pharmacokinetics, and clinical efficacy and safety are reviewed in Chemotherapy (Tokyo), 33, Suppl. 7, 1-1024 (1985) and in Symposium on antibacterial spectrum and clinical use: Am. J. Med. 82, Suppl., 4A, 1-404 (1987). ##STR7##
Ofloxacin, (2) (.+-.)-9-fluoro-2,3-drhydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H- pyrido1,2,3-de!-1,4-benzoxazine-6-carboxylic acid, is another analogue of norfloxacin. The medicinal chemistry of ofloxacin is reported in Imamaura et. al., Antimicrob. Agents Chemother. 1987, 31, 325 and in Daichi, S. Drugs Future, 1983, 8, 395. ##STR8##
Lomefloxacin, 1-ethyl-6,8-difluoro-1,4-dihydro-4-oxo-7-(3-methyl-1-piperazinyl)-3-quinol inecarboxylic acid, is another close analogue of norfloxacin. Its preparation has been reported in U.S. Pat. No. 4,528,287 and the biological properties of the compound are reported by T. Hirose et. al., in Antimicrob. Ag. Chem.ther. 31, 854, 1987. ##STR9##
Norfloxacin, Ciprofloxacin, Ofloxacin, Lomefloxacin are approved oral antibacterials.